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Angiogenesis PDGFR Tivozanib

Tivozanib

Catalog No. T2456   CAS 475108-18-0
Synonyms: KRN951, AV-951

Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

Tivozanib, CAS 475108-18-0
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 75.00
10 mg In stock 100.00
25 mg In stock 200.00
50 mg In stock 280.00
100 mg In stock 500.00
1 mL * 10 mM (in DMSO) In stock 81.00
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Purity 97.41%
Purity 99.33%
Purity 98.23%
Biological Description
Chemical Properties
Storage & Solubility Information
Preparing Solutions
Description Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
Targets&IC50 EphB2 : ic50 24nM ,   PDGFRα : ic50 40nM ,   VEGFR1 : ic50 30nM ,   VEGFR2 : ic50 6.5nM ,   VEGFR3 : ic50 15nM
Kinase Assay Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1.
Cell Research
Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts-based assays are done to determine the ability of AV-951 to inhibit ligand-dependent phosphorylation of tyrosine kinase receptors. The cells are starved overnight in appropriate basic medium containing 0.5% fetal bovine serum (FBS). The cells are incubated for 1 hour following the addition of AV-951 or 0.1% DMSO, and then stimulated with the cognate ligand at 37 °C. Receptor phosphorylation is induced for 5 minutes except for VEGFR3 (10 minutes), c-Met (10 minutes), and c-Kit (15 minutes). All the ligands used in the assays are human recombinant proteins, except for VEGF-C, a rat recombinant protein. Following cell lysis, receptors are immunoprecipitated with appropriate antibodies and subjected to immunoblotting with phosphotyrosine. Quantification of the blots and calculation of IC50 values are carried ou(Only for Reference)
Cell lines: Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts
Animal Research
Animal Model: A549 xenografts in Athymic rats (RH-rnu/rnu)
Synonyms KRN951 , AV-951
Purity 97.41%
Molecular Weight 454.86
Formula C22H19ClN4O5
CAS No. 475108-18-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 16 mg/mL (35.2 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% methylcellulose: 30 mg/mL

Citations

References and Literature
1. Nakamura K, et al. Cancer Res, 2006, 66(18), 9134-9142. 2. Taguchi E, et al. Cancer Sci, 2008, 99(3), 623-630.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Tyrosine kinase inhibitor library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library

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